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采用Stober法合成了氨基修饰的阳离子介孔硅纳米粒(CMSN)。所得的CMSN呈圆整球形、介孔明显,粒径为(98.4±2.8)nm,ζ电位为(13.2±1.8)m V,在0~20mg/ml范围内对Caco-2细胞无明显的细胞毒性。以CMSN为载体,采用饱和溶液吸附法反复吸附葛根素(1)7次达到满载,载药量约为18%。在含有2%十二烷基硫酸钠的磷酸盐缓冲液(pH7.4)中,1-CMSN中1的体外释药行为符合Weibull模型(R~2=0.923 6)。Caco-2肠壁单层模型中,1-CMSN的跨膜吸收和分泌表观渗透系数P_(app)(×10~(-6) cm/s)为23.89±1.22和17.03±1.21,流出率(ER)为1.403,与1原料药有显著差异(P<0.05)。
Amino modified cationic mesoporous silica nanoparticles (CMSN) were synthesized by Stober method. The resulting CMSN was spherical and well-mesopore with a diameter of (98.4 ± 2.8) nm and a zeta potential of (13.2 ± 1.8) mV. No obvious cells were observed in Caco-2 cells in the range of 0-20 mg / ml toxicity. With CMSN as the carrier, puerarin (1) was adsorbed repeatedly for seven times by saturated solution adsorption method, and the drug loading was about 18%. The in vitro release behavior of 1-CMSN1 was in accordance with the Weibull model (R ~ 2 = 0.923 6) in phosphate buffered saline (pH 7.4) containing 2% sodium dodecyl sulfate. In Caco-2 model of intestinal wall monolayer, the transmembrane absorption and excretion apparent permeability coefficient P_ (app) (× 10 ~ (-6) cm / s) of 1-CMSN were 23.89 ± 1.22 and 17.03 ± 1.21, (ER) was 1.403, which was significantly different from 1 API (P <0.05).